6-甲氧基-3-吡啶羧胺
| 中文名称 | 6-甲氧基-3-吡啶羧胺 |
|---|---|
| 中文同义词 | 6-甲氧基-3-吡啶羧胺;6-甲氧基-3-吡啶甲酰胺;化合物JBSNF-000088;6-甲氧基烟酰胺;化合物JBSNF-000088,10 MM DMSO 溶液 |
| 英文名称 | 6-Methoxynicotinamide |
| 英文同义词 | 6-Methoxynicotinamide;3-PYRIDINECARBOXAMIDE, 6-METHOXY-;6-METHOXYPYRIDINE-3-CARBOXAMIDE;BUTTPARK 182\12-94;JBSNF-000088;JBSNF-000088 (JBSNF000088;6-methoxy-3-pyridinecarboxamide;Inhibitor,JBSNF 000088,inhibit,6-Methoxynicotinamide,JBSNF-000088 |
| CAS号 | 7150-23-4 |
| 分子式 | C7H8N2O2 |
| 分子量 | 152.15 |
| EINECS号 | 604-604-1 |
| 相关类别 | |
| Mol文件 | 7150-23-4.mol |
| 结构式 |  |
6-甲氧基-3-吡啶羧胺 性质
| 熔点 | 178-180°C |
|---|---|
| 沸点 | 301.6±22.0 °C(Predicted) |
| 密度 | 1.213±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C Freezer |
| 溶解度 | 可溶于DMSO（少许）、甲醇（少许） |
| 形态 | 固体 |
| 酸度系数(pKa) | 15.17±0.50(Predicted) |
| 颜色 | 灰白色至浅米色 |
| InChI | InChI=1S/C7H8N2O2/c1-11-6-3-2-5(4-9-6)7(8)10/h2-4H,1H3,(H2,8,10) |
| InChIKey | KXDSMFBEVSJYRF-UHFFFAOYSA-N |
| SMILES | C1=NC(OC)=CC=C1C(N)=O |
| Target | Value |
|
hNNMT
(Cell-free assay) | 1.8 μM |
|
mkNNM
(Cell-free assay) | 2.8 μM |
|
mNNMT
(Cell-free assay) | 5.0 μM |
JBSNF-000088 (6-Methoxynicotinamide) has IC 50 values are 1.6 and 6.3 µM for U2OS or differentiated 3T3L1 cells.
JBSNF-000088 (6-Methoxynicotinamide) (50 mg/kg; oral route of administration for four weeks) shows statistically significant reduction in body weight (%) and leads to a statistically significant reduction in fed blood glucose on day 21.
JBSNF-000088 (50 mg/kg; oral gavage administration; twice daily for four weeks) leads to a statistically significant improvement in oral glucose tolerance on day 28 with glucose tolerance being normalized.
JBSNF-000088 (1 mg/kg; intravenous administration; for 4 hours) results in low plasma clearance of 21 mL/min▪kg and the volume of distribution at steady state of 0.7 L/kg, a very short plasma half-life of 0.5 hours upon intravenous administration.
JBSNF-000088 (10 mg/kg; oral gavage; for 4 hours) results in a Cmax of 3568 ng/mL with a T
max
value of 0.5 hours, indicating rapid absorption in the intestine, and half-life of 0.4 hours by oral gavage. The oral bioavailability is found to be approximately 40%.
| Animal Model: | Mice with high fat diet (HFD)-induced obesity |
| Dosage: | 50 mg/kg |
| Administration: | Oral route of administration for four weeks; oral gavage administration and twice daily for four weeks |
| Result: |
Showed statistically significant reduction in body weight (%) and led to a statistically significant reduction in fed blood glucose on day 21 by oral route of administration.
Led to a statistically significant improvement in oral glucose tolerance on day 28 with glucose tolerance being normalized by oral gavage administration. |
| Animal Model: | C57BL/6 mice |
| Dosage: | 1 mg/kg (Intravenous administration);10 mg/kg (oral gavage)(Pharmacokinetic Study) |
| Administration: | Intravenous administration and oral gavage; for 4 hours |
| Result: |
Resulted in low plasma clearance of 21 mL/min▪kg and the volume of distribution at steady state of 0.7 L/kg, a very short plasma half-life of 0.5 h upon intravenous administration.
Resulted in a Cmax of 3568 ng/mL with a T max value of 0.5 hours, indicating rapid absorption in the intestine, and half-life of 0.4 hours by oral gavage. |
安全信息
| WGK Germany | WGK 3 |
|---|---|
| 海关编码 | 2933399990 |
| 存储类别 | 11 - 可燃固体 |
| 危险性类别 | 眼部刺激 类别2 |